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31. 发明授权

US5399710A Protein labeling reagents 失效
公开(公告)号：US5399710A
公开(公告)日：1995-03-21
申请号：US994939
申请日：1992-12-22
申请人： Sudhakar Kasina , Ananthachari Srinivasan , James Sanderson , Alan R. Fritzberg
发明人： Sudhakar Kasina , Ananthachari Srinivasan , James Sanderson , Alan R. Fritzberg
IPC分类号： A61K51/10 , C07C319/18 , C07C323/52 , C07D307/60 , C07D339/06 , C07D495/04 , C07D487/04 , C07D207/38 , C07C101/04
CPC分类号： C07D495/04 , A61K51/1093 , C07C319/18 , C07D307/60 , C07D339/06 , A61K2123/00 , Y02P20/55
摘要： Novel labeling reagents are useful for radiolabeling proteins such as antibodies with radionuclide metals such as .sup.99m Tc, .sup.186 Re, and .sup.188 Re. The reagents are of the following formula: ##STR1## wherein: each X is independently chosen from O, S, NH, or NR.sub.2, wherein R.sub.2 is a protecting group or an electron withdrawing group;R.sub.1 represents a protecting group, wherein each R.sub.1 is a separate protecting group or the two R.sub.1 symbols are taken together to represent a single protecting group; andeach T is independently chosen from hydrogen, lower alkyl groups of from 1 to about 6 carbon atoms, electron withdrawing groups, and lower alkyl groups of from 1 to about 6 carbon atoms substituted with electron withdrawing group(s).

32. 发明授权

US5250666A Radionuclide metal chelates for the radiolabeling of proteins 失效
标题翻译：放射性核素金属螯合物用于放射性标记蛋白质
公开(公告)号：US5250666A
公开(公告)日：1993-10-05
申请号：US973048
申请日：1992-11-06
申请人： Linda M. Gustavson , Ananthachari Srinivasan , Sudhakar Kasina , Alan R. Fritzberg
发明人： Linda M. Gustavson , Ananthachari Srinivasan , Sudhakar Kasina , Alan R. Fritzberg
IPC分类号： A61K51/10 , C07D263/26 , C07D309/08 , C07D327/04 , C07F13/00 , C07K5/06 , A61K43/00
CPC分类号： C07K5/0606 , A61K51/1093 , C07D263/26 , C07D309/08 , C07D327/04 , C07F13/005 , A61K2123/00
摘要： Chelating compounds of specified structure are useful for radiolabeling targeting proteins such as antibodies. The radiolabeled antibodies, or catabolites thereof, demonstrate improved biodistribution properties, including reduced localization within the intestines.
摘要翻译：特定结构的螯合化合物可用于放射性标记靶向蛋白如抗体。放射性标记的抗体或其分解代谢物表现出改善的生物分布特性，包括减少肠内定位。

33. 发明授权

US5112953A Radiolabeled proteins for diagnostic or therapeutic use 失效
标题翻译：放射性蛋白质用于诊断或治疗用途
公开(公告)号：US5112953A
公开(公告)日：1992-05-12
申请号：US457480
申请日：1989-12-29
申请人： Linda M. Gustavson , Ananthachari Srinivasan , Sudhakar Kasina , John M. Reno , Jeffrey N. Fitzner , David S. Jones
发明人： Linda M. Gustavson , Ananthachari Srinivasan , Sudhakar Kasina , John M. Reno , Jeffrey N. Fitzner , David S. Jones
IPC分类号： A61K51/00 , A61K38/00 , A61K47/48 , A61K51/10 , A61P35/00 , C07D207/46 , C07D309/08 , C07K1/107 , C07K5/06 , C07K5/08 , C07K5/083 , C07K14/00 , C07K14/52 , C07K14/575 , C07K16/00 , C09K3/00 , G01N33/534 , G01N33/577
CPC分类号： C07K5/0606 , A61K47/48707 , A61K51/1093 , C07D207/46 , C07D309/08 , C07K5/0806 , A61K38/00
摘要： Chelating compounds of specified structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.
摘要翻译：特定结构的螯合化合物可用于放射性标记靶向分子如抗体。可切割接头将放射性核素金属螯合物连接到抗体上。放射标记的抗体具有改善的生物分布特性，包括减少肠和肾内的定位。

34. 发明授权

US5106951A Antibody conjugates 失效
标题翻译：抗体结合
公开(公告)号：US5106951A
公开(公告)日：1992-04-21
申请号：US332610
申请日：1989-03-31
申请人： Alton C. Morgan, Jr. , Ananthachari Srinivasan , John M. Reno , Alan R. Fritzberg , David C. Anderson
发明人： Alton C. Morgan, Jr. , Ananthachari Srinivasan , John M. Reno , Alan R. Fritzberg , David C. Anderson
IPC分类号： A61K31/495 , A61K31/505 , A61K31/675 , A61K31/70 , A61K39/395 , A61K47/48 , A61P35/00 , C07K14/00 , C07K16/00
CPC分类号： A61K47/48369 , A61K47/48384
摘要： There is disclosed an antibody and antibody-drug conjugate for targeting drug delivery as well as a class of chemicals, termed a drug-binding molecule of complementary structure (csDBM). The csDBM is designed to "fit" the drug by combining multiple non-covalent interactions between functional groups on the drug and opposing functional groups on the csDBM. The net result on the antibody-csDBM-drug conjugate is a drug stably bound to the csDBM so as not to dissociate during in vivo administration, but not so tightly bound to allow drug dissociation from the conjugate without significant loss of activity and retaining the drug's ability to bind to a higher affinity site on or within the target cell.

35. 发明授权

US5091514A Metal-radionuclide-labeled proteins and glycoproteins for diagnosis and therapy 失效
标题翻译：用于诊断和治疗的金属放射性核素标记的蛋白质和糖蛋白
公开(公告)号：US5091514A
公开(公告)日：1992-02-25
申请号：US494191
申请日：1990-03-15
申请人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
发明人： Alan R. Fritzberg , Sudhakar Kasina , Tripuraneni N. Rao , Jean-Luc VanderHeyden , Ananthachari Srinivasan
IPC分类号： A61K51/04 , A61K51/08 , A61K51/10 , C07B59/00 , C07F13/00 , G01N33/534
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/088 , A61K51/1066 , A61K51/1093 , C07B59/004 , C07F13/005 , A61K2121/00 , A61K2123/00
摘要： Chelated radionuclide compositions are provided for conjugation to polypeptides and carbohydrates. The resulting conjugates may be used in diagnosis and therapy.
摘要翻译：螯合放射性核素组合物用于与多肽和碳水化合物结合。所得到的缀合物可用于诊断和治疗。

36. 发明授权

US5021556A Method of radiolabeling chelating compounds comprising sulfur atoms with metal radionuclides 失效
标题翻译：包含硫原子的螯合化合物与金属放射性核素放射性标记的方法
公开(公告)号：US5021556A
公开(公告)日：1991-06-04
申请号：US212688
申请日：1988-07-01
申请人： Ananthachari Srinivasan
发明人： Ananthachari Srinivasan
IPC分类号： A61K51/04 , C07C323/60 , C07C327/24 , C07D285/00 , C07D309/08 , C07F13/00 , C07H15/14
CPC分类号： C07D285/00 , A61K51/0478 , A61K51/0491 , C07C323/60 , C07C327/24 , C07D309/08 , C07F13/005 , C07H15/14 , A61K2123/00 , Y02P20/55
摘要： Chelating compounds which comprise one or more sulfur atoms and are to be radiolabeled with metal radionuclides to form the corresponding chelates are disclosed. The chelating compounds comprise thioacetal or hemithioacetal sulfur protecting groups which are displaced during the radiolabeling reaction, which is conducted at acidic pH, such that bonds form between said sulfur atoms and said radionuclide. The resulting metal radionuclide chelates have diagnostic and therapeutic medical uses.
摘要翻译：公开了包含一个或多个硫原子并且与金属放射性核素进行放射性标记以形成相应螯合物的螯合化合物。螯合化合物包括在酸性pH下进行的放射性标记反应期间被置换的硫代缩醛或半硫缩醛硫保护基，使得在所述硫原子和所述放射性核素之间形成键。所得金属放射性核素螯合物具有诊断和治疗用途。

37. 发明授权

US4897255A Metal radionuclide labeled proteins for diagnosis and therapy 失效
公开(公告)号：US4897255A
公开(公告)日：1990-01-30
申请号：US65011
申请日：1987-06-19
申请人： Alan R. Fritzberg , Sudhakar Kasina , Ananthachari Srinivasan , Daniel S. Wilbur
发明人： Alan R. Fritzberg , Sudhakar Kasina , Ananthachari Srinivasan , Daniel S. Wilbur
IPC分类号： A61K51/04 , A61K51/10 , A61K51/12 , C07C227/08 , C07C271/22
CPC分类号： C07C271/22 , A61K51/0478 , A61K51/1093 , A61K51/12 , B82Y5/00 , C07C227/08 , A61K2123/00 , Y10S530/866
摘要： Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficiently.

38. 发明授权

US06866837B2 Radiolabeled peptides for the diagnosis and treatment of breast and prostate tumors and metastases of such tumors 失效
标题翻译：放射性标记的肽用于诊断和治疗乳腺和前列腺肿瘤以及这种肿瘤的转移
公开(公告)号：US06866837B2
公开(公告)日：2005-03-15
申请号：US10248668
申请日：2003-02-06
申请人： Jean-Claude Reubi , Wout A. Breeman , Ananthachari Srinivasan
发明人： Jean-Claude Reubi , Wout A. Breeman , Ananthachari Srinivasan
IPC分类号： A61K38/00 , C07K7/08 , A61K51/00
CPC分类号： C07K7/086 , A61K38/00
摘要： Compounds and methods for the diagnosis and treatment of tumors, including breast and prostate tumors and metastases thereof using radiolabelled peptides that bind to GRP receptors. The peptides are Bombesin analogs wherein the first and optionally the third amino acid are modified.
摘要翻译：使用与GRP受体结合的放射性标记肽来诊断和治疗肿瘤的化合物和方法，包括乳腺和前列腺肿瘤及其转移。所述肽是Bombesin类似物，其中第一个和任选的第三个氨基酸被修饰。

39. 发明授权

US6132697A Radiopharmaceutical compositions capable of localizing at sites of thrombus 失效
标题翻译：可以在血栓位置定位的放射性药物组合物
公开(公告)号：US6132697A
公开(公告)日：2000-10-17
申请号：US870042
申请日：1997-06-05
申请人： Ananthachari Srinivasan , Larry P. Feigen , Daniel Lee Flynn , Jeffery Alan Zablocki , Philip Needleman , Michelle A. Schmidt
发明人： Ananthachari Srinivasan , Larry P. Feigen , Daniel Lee Flynn , Jeffery Alan Zablocki , Philip Needleman , Michelle A. Schmidt
IPC分类号： A61K38/00 , A61K51/00 , A61K51/08 , C07K5/072 , C07F5/00
CPC分类号： C07K5/06113 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.
摘要翻译：提供了能够在哺乳动物体内含有活化血小板的血栓位点定位的放射性药物，其中放射性药物包含能够特异性结合血栓中血小板的GPIIb / IIIa整联蛋白受体的线性拟肽含量配体和共价结合的放射性核素含有拟肽的配体。提供本发明的配体组合物与所选择的金属放射性核素复合以形成诊断或治疗性放射性药物，以分别对血栓位点成像或向血栓部位提供放射治疗。通过施用诊断上有效量的本发明的放射性药物组合物与选定的诊断性金属放射性核素复合而在哺乳动物体内成像血栓位点的方法和通过施用治疗有效的方法向哺乳动物体内的血栓位点提供治疗还提供了与选定的治疗性金属放射性核素复合的本发明的放射性药物组合物的量以及用于制备这种放射性药物组合物的试剂盒。

40. 发明授权

US5830431A Radiolabeled peptide compositions for site-specific targeting 失效
标题翻译：用于位点特异性靶向的放射性标记肽组合物
公开(公告)号：US5830431A
公开(公告)日：1998-11-03
申请号：US480373
申请日：1995-06-07
申请人： Ananthachari Srinivasan , Mary Marmion Dyszlewski , Joseph E. Bugaj , Jack L. Erion
发明人： Ananthachari Srinivasan , Mary Marmion Dyszlewski , Joseph E. Bugaj , Jack L. Erion
IPC分类号： A61K51/00 , A61K51/08 , A61P35/00 , C07K14/655 , A61M36/14
CPC分类号： C07K14/6555 , A61K51/083 , A61K51/088
摘要： This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.
摘要翻译：本发明涉及用于放射性药物用途的放射性标记肽组合物，更具体地，涉及具有未修饰的羧基末端氨基酸的用于诊断或治疗用途的放射性标记肽。放射性药物组合物可以用于靶向选定的生物部位。放射性标记的肽的特征在于其羧基末端氨基酸为羧酸形式，肽通过螯合剂偶联至诊断或治疗放射性核素。放射性药物组合物优选包含选自生长抑素，生长抑素类似物，生长抑素衍生物和能够结合生长抑素受体的肽的放射性标记的肽，其中肽通过螯合剂偶联至诊断或治疗放射性核素其羧基末端氨基酸呈羧酸形式。

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